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48 Cards in this Set
- Front
- Back
decreased Km
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increased affinity
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Competitive inhibitor on 1/v;1/s graph
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"competitively crosses" the uninhibited drug line at the y intercept; lesser affinity, same vmax
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noncompetitive inhibitor on the 1/v;1/s graph
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noncompetitor, noncrossing; shares x-intercept with uninhibited; same Km, lesser vmax
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volume of distribution
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amount of drug in the body/plasma drug concentration
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clearance
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rate of drug elimination/plasmadrug concentration
or volume of distribution/elimination constant |
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half-life equation; drug infusion
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(.7xVolume of distribution)/clearance
a drug infused at constant rate reaches 94% of steady state in 4 half lives |
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loading dose equation
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=Cp x Vd/F (Cp is target plasma level and F is bioavailability)
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Maintenance dose
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=Cp x CL/F
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Zero order elimination (give examples)
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constant rate of elimination
PEA - Phanytoin, Ethanol, Aspirin PEAs are round like a Zero |
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First Order elimination
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constant Fraction of drug is eliminated per unit time
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effect of an antagonist
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decreases potency, (more drug required for the same effect)
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effect of a non-competitive antagonist
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decreases efficacy (decreases the maximal effect possible by the agonist-drug)
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partial agonists
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have a LOWER MAXIMAL EFFECT/EFFICACY; may have a lower, higher or identicle potency (based on the EC50 of the full agonist).
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Therapeutic index
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TILE: TI = Ld50/Ed50 (toxic dose and effective doe respectively); safer drugs have a higher TI
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G-protein linked second messengers.
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KISS and KICK til you're SICK of SEX
QISS and QIQ til you're SIQ of SQS Order: a1b1a2b2; m1m2m3; d1d2h1; h2v1v2 |
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a1
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q: vasoconstriction; pupil dilation
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a2
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i: decreases both sympathetic outflow and insulin release
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b1
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s: increases heart rate contractility, renin release, and lipolysis
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b2
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s: vaso/broncho dilation; increases HR contractility, lipolysis, glucagon release
decreases uterine tone |
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m1
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q: CNS, enteric nervous system
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m2
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i: decreases HR and contractility
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m3
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q: increases exocrine secretion, gut peristalsis, bladder contraction, bronchoconstriction; increases pupillary sphincter tone (miosis) and ciliary contraction (accomodation
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d1
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s: relaxes renal vascular smooth muscle
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d2
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i: modulares transmitter release, esp. in the brain
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h1
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q: increases nasal and bronchial mucus, contraction of the bronchioles, pruritis, pain
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h2
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s: increases gastric acid secretion
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v1
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q: vascular smooth muscle contraction
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v2
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s: increases H2O permeability and reabsorption in the collecting tubules of the kidney
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Gq receptor types
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HAVe 1 M&M - H1, a1, V1, M1, M3
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Gs receptor types
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stimulated To(2) BeHaVe BaD1y - B2, H2, V2, B1, D1
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Gi receptor Types:
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MAD 2's: M2 a2 D2
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Cholinergic syndromes
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Over-stimulation of ACh receptors:
DUMBBELSS: diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skm/cns, lacrimation, sweating, salivation |
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treatment of Cholinergic syndrome
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atropine (M antagonist) and pralidoxime (regenerates cholinesterase)
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selective B2 agonists
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MAST - metaprotenerol, albuterol, salmeterol, terbutaline
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B1-antagonists
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A BEAM of B1-blockers: Acebutolol, Betaxolol, Esmolol, Atenolol, Metoprolol
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B1/B2 antagonists
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Tim and Nadine Pin a Label on their Property: Timolol, Nadolol, Pindolol, Labetolol, Propranolol
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Therapeutic Index
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TILE: TI = LD50/ED50
increased TI = increased safety |
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zero order elimination
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PEA: phenytoin Ethanol Aspirin
elimination decreases linearly with time |
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First order elimination
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Fractional elimination with time causing an exponential decrease in [plasma]
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P450 Inducers
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Queen Barb was INDUCED to Steal Phen-phen and Refuse Greasy Carbs
Queen - quinidine Barb - Barbiturates Steals - St. Johns Wood Phen-Phen (and) - Phenytoin Refuses - Rifampin Greasy - Greseofulvan Carbs - Carbamazapine |
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P450 Inhibitors
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Drink from a KEG and get SICk and INHIBITED
Ketoconazol Erythromycin (macrolids except azithro) Grapefruit juice Sulfonamides Isoniazid Cimetidine |
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Drugs contraindicated in Pregnancy
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SAFE Moms Take Really Good Care
Sulfonamides - kernicterus Aminoglycosides - ototoxicity Fluoroquinolones - cartilaginous damage Erythromycin - acute cholestatis hepatitis in Mom and Clarithromycin is embryotoxic Metronidazol - Mutagenesis Tetracyclin - teeth colored and bone problems Ribavirin - teratogen Gresiofulvan - teratogen Chloramphenical - Grey Baby Syndrome Also warfarin |
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Bacteriostatic drugs
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ECSTaTiC
Erythromycin Clindamycin Sulfamethoxazole Trimethoprim Tetracyclins Chloramphenicol |
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Bacterocidal drugs
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Very Finely Proficient At Cell Murder
Vancomycin Fluoroquinolones Penicillin Aminoglycosides Cephalosporine Metronidazol |
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what is MAC
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anesthetics: minimal alveolar concentration at which 50% of the population is anesthetized...it decreases with age.
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how does MAC relate to potency
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potency = 1/MAC
decreased MAC means increased potency and visa versa |
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Blood solubility relates to what?
give example of the relationship |
induction and recovery.
decreased blood solubility = rapid induction and rapid recovery increased blood solubility = slow induction and slow recovery |
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lipid solubility relates to what?
give an example of the relationship |
potency and MAC
increased lipid solubility means increased potency and therefore decreased MAC. |